H-151 ( —— )

产品货号. M20369 CAS No. 941987-60-6

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

H-151
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

H-151 是一种高效、选择性的 STING 共价拮抗剂，可降低 TBK1 磷酸化并抑制人 STING 棕榈酰化。
产品描述

H-151 is a highly potent selective and covalent antagonist of?STING reduces TBK1 phosphorylation and suppresses human STING palmitoylation.(In Vitro):H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells.H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells.H-151 (1 μM; 3 h) suppresses hsSTING palmitoylation.(In Vivo):H-151 (750 nmol per mouse; a single i.p.) markedly reduces systemic cytokine responses in CMA-treated mice.H-151 (750 nmol per mouse; i.p. daily for 7 d) exhibits notable efficacy in Trex1?/? mice that expressed a bioluminescent IFNβ reporter.H-151 (750 nmol per mouse; i.p.) reaches effective systemic levels, displays a short half-life in the serum and forms an adduct to mmSTING in wild-type mice.
体外实验

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体内实验

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同义词

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通路

Immunology/Inflammation
靶点

STING
受体

STING
研究领域

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适应症

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1.Haag S M Gulen M F Luc R et al. Targeting STING with covalent small-molecule inhibitors[J]. Nature 2018.

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